1. Zhejiang Academy of Medical Sciences, Hangzhou 310013, China; 2. Department of Pharmacy, Zhejiang Chinese Medicine University, Hangzhou 310053, China
Abstract��OBJECTIVE To prepare huperzine A micro-porous osmotic pump pellets and to investigate the pharmacokinetic properties in Beagle dogs. METHODS The extrusion-spheronisation method was used to prepare the core of huperzine A pellets which then coated by fluid-bed coating technology.Central composite design-response surface method was used to optimize the prescription of coating layer.Then Zero-order, First-order and Higuchi equation of cumulative release with time were fitted to study its release characteristics.The commercially available huperzine A tablets were used as reference preparations to investigate the in vivo pharmacokinetics of huperzine A micro-porous osmotic pump pellets, and the bioequivalence of the two preparations were compared. RESULTS The formula of coating was optimized as followsEC of 61.5%, PEG400 of 10.5%. Zero-order kinetics existed in the release of the pellets in 24 h. Moreover, the osmotic pressure-controlled delivery was greatly responsible for drug release. In vivo study showed that tmax and ��max of huperzine A micro-porous osmotic pump pellets were significantly lower than that of the reference preparation, and its t1/2 was significantly prolonged compared with the reference preparation, the relative bioavailability was 95.8%. CONCLUSION Huperzine A micro-porous osmotic pump pellets had a better sustained release effect in the Beagle dog and have a good correlation in vivo.
XU H B, WANG X P, LIU B L. Pharmacological studies and clinical application of huperzine A. World Clin Drugs(�����ٴ�ҩ��),2014, 35(1):60-63.
[2]
WANG R, YAN H, TANG X C. Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine . Acta Pharmacol Sin(�й�ҩ��ѧ��), 2006, 27(1):1-26.
[3]
CHEN X Q, JIN Y Y, TANG G, et al. Handbook of New Pharmacology(�±�ҩ��ѧ) Vol.17. Beijing:People��s Medical Publishing House, 2011:318.
[4]
WANG W P, XIE X Q, YANG D J, et al. Osmotically controlled oral drug delivery systems:an update review. China J Chin Mater Med(�й���ҩ��־), 2008, 5(33):598-602.
[5]
MA L. Progress in osmotic pump drug delivery system. J Chin Pharm Univ(�й�ҩ�ƴ�ѧѧ��), 2014, 45(6):726-730.
[6]
LIU H, ZHANG J, XU S. Formulation screening and in vitro dissolution model fitting of bupropion hydrochloride microporous osmotic pump tablets . Chin Pharm J(�й�ҩѧ��־), 2011,46(15):1179-1183.
[7]
XU X H, LIAO L Y, JIANG T. Release mechanism of PNS microporous membrane osmotic pump tablets . Chin J Exp Tradit Med Form(�й�ʵ�鷽��ѧ��־),2012,18(8):12-14.
[8]
FANG Y, XIANG B, PAN Z H,et al. Preparation and dissolution test in vitro of matrine controlled porosity osmotic pump tablet. Chin Tradit Pat Med(�г�ҩ),2010,32(5):750-753.
[9]
JIN L Y, ZHANG Z, HAN F. Effects of coating on the in vitro release character of venlafaxine hydrochloride microporous membrane osmotic pump tablets. J Shenyang Pharm Univ(����ҩ�ƴ�ѧѧ��), 2008, 25(8):593-597.
[10]
WU X J, LIU W N, WANG J, et al. Preparation of nefopamrosity osmotic pump by hydrochloride controlled pocentral composite design. J Shenyang Pharm Univ (����ҩ�ƴ�ѧѧ��), 2009, 26(11):863-867.
[11]
Ch.P(2015) Vol��(�й�ҩ��2015���,����). 2015:163.
[12]
RAHMAN M A, AHUJA A, BABOOTA S, et al. Recent advances in pelletization technique for oral delivery: a review. Curr Drug Deliv, 2009, 6(1):122-129.
[13]
CHEBOYINA S, WYANDT C M. Wax-based sustained release matrix pellets prepared by a novel freeze pelletization technique ��: in vitro drug release studies and release mechanisms. Int J Pharm, 2008, 359 (1/2):167-173.
2019, Vol. 54 
